• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

氯卡色林。用于肥胖症:存在不可接受的风险。

Lorcaserin. In obesity: unacceptable risks.

出版信息

Prescrire Int. 2014 May;23(149):117-20.

PMID:24926508
Abstract

Treatment of obesity and overweight is based primarily on dietary measures and physical exercise.There are still no drugs with a favourable harm-benefit balance in this setting. Lorcaserin, a "selective" 5HT2C serotonin receptor agonist, has been refused marketing authorisation in the European Union despite approval in the United States. Clinical evaluation of lorcaserin is based on three placebo-controlled trials, each lasting one year, in a total of about 6000 patients. Two trials involved obese patients, and one obese patients with type 2 diabetes. The results of these trials are undermined by the large proportion (40% to 50%) of patients who were lost to follow-up before the end of the trial. None of the trials examined the impact of lorcaserin on the clinical complications of obesity. From an average initial weight of about 100 kg, patients taking lorcaserin lost only about 3 kg more than those in the placebo groups.The patients put on weight again after lorcaserin was discontinued. Adverse effects observed in clinical trials were mainly gastrointestinal (dry mouth, nausea) and neuropsychiatric (dizziness, fatigue, headache, euphoria). The incidence of cardiac valve disorders was higher with lorcaserin than with placebo. These trials were too short in duration to exclude a risk of cancer (breast cancer and astrocytoma) that was reported in experimental animals. This serotonin agonist is metabolised by the liver, creating a risk of multiple drug interactions. In practice, lorcaserin has not been shown to prevent complications of obesity or even lead to substantial weight loss.There is therefore no justification for exposing patients to the risk of adverse effects.

摘要

肥胖和超重的治疗主要基于饮食措施和体育锻炼。在这种情况下,仍然没有危害效益比良好的药物。洛卡塞林是一种“选择性”5-羟色胺2C(5HT2C)受体激动剂,尽管在美国已获批准,但在欧盟仍未获得上市许可。洛卡塞林的临床评估基于三项安慰剂对照试验,每项试验持续一年,总共约6000名患者。两项试验涉及肥胖患者,一项涉及肥胖的2型糖尿病患者。这些试验的结果受到很大比例(40%至50%)的患者在试验结束前失访的影响。没有一项试验研究洛卡塞林对肥胖临床并发症的影响。服用洛卡塞林的患者平均初始体重约为100公斤,仅比安慰剂组的患者多减轻约3公斤。停用洛卡塞林后,患者体重又增加了。临床试验中观察到的不良反应主要是胃肠道反应(口干、恶心)和神经精神反应(头晕、疲劳、头痛、欣快感)。服用洛卡塞林的患者心脏瓣膜疾病的发生率高于服用安慰剂的患者。这些试验持续时间过短,无法排除实验动物中报告的癌症(乳腺癌和星形细胞瘤)风险。这种5-羟色胺激动剂由肝脏代谢,存在多种药物相互作用的风险。实际上,洛卡塞林并未显示出能预防肥胖并发症,甚至也未导致显著体重减轻。因此,没有理由让患者承受不良反应的风险。

相似文献

1
Lorcaserin. In obesity: unacceptable risks.氯卡色林。用于肥胖症:存在不可接受的风险。
Prescrire Int. 2014 May;23(149):117-20.
2
A one-year randomized trial of lorcaserin for weight loss in obese and overweight adults: the BLOSSOM trial.一项为期一年的用于肥胖和超重成年人减肥的lorcaserin 随机试验:BLOSSOM 试验。
J Clin Endocrinol Metab. 2011 Oct;96(10):3067-77. doi: 10.1210/jc.2011-1256. Epub 2011 Jul 27.
3
Lorcaserin: an investigational serotonin 2C agonist for weight loss.氯卡色林:一种用于减肥的研究性 5-羟色胺 2C 激动剂。
Am J Health Syst Pharm. 2011 Nov 1;68(21):2029-37. doi: 10.2146/ajhp100638.
4
Safety and tolerability review of lorcaserin in clinical trials.氯卡色林在临床试验中的安全性和耐受性评估
Clin Obes. 2016 Oct;6(5):285-95. doi: 10.1111/cob.12159.
5
The safety and efficacy of lorcaserin in the management of obesity.盐酸氯卡色林治疗肥胖症的安全性和有效性。
Postgrad Med. 2013 Nov;125(6):62-72. doi: 10.3810/pgm.2013.11.2713.
6
Lorcaserin: drug profile and illustrative model of the regulatory challenges of weight-loss drug development.洛卡塞林:减肥药研发监管挑战的药物概况及示例模型
Expert Rev Cardiovasc Ther. 2011 Mar;9(3):265-77. doi: 10.1586/erc.10.22.
7
Cardiovascular Safety of Lorcaserin in Overweight or Obese Patients.盐酸氯卡色林在超重或肥胖患者中的心血管安全性。
N Engl J Med. 2018 Sep 20;379(12):1107-1117. doi: 10.1056/NEJMoa1808721. Epub 2018 Aug 26.
8
Multicenter, placebo-controlled trial of lorcaserin for weight management.多中心、安慰剂对照的氯卡色林用于体重管理的试验。
N Engl J Med. 2010 Jul 15;363(3):245-56. doi: 10.1056/NEJMoa0909809.
9
Design and rationale for the Cardiovascular and Metabolic Effects of Lorcaserin in Overweight and Obese Patients-Thrombolysis in Myocardial Infarction 61 (CAMELLIA-TIMI 61) trial.罗西司琼在超重和肥胖患者中心血管和代谢影响的设计和原理-心肌梗死溶栓治疗 61 号试验(CAMELLIA-TIMI 61 试验)。
Am Heart J. 2018 Aug;202:39-48. doi: 10.1016/j.ahj.2018.03.012. Epub 2018 Mar 29.
10
Echocardiographic assessment of cardiac valvular regurgitation with lorcaserin from analysis of 3 phase 3 clinical trials.使用 lorcaserin 进行 3 项 3 期临床试验的心脏瓣膜反流的超声心动图评估。
Circ Cardiovasc Imaging. 2013 Jul;6(4):560-7. doi: 10.1161/CIRCIMAGING.112.000128. Epub 2013 May 9.

引用本文的文献

1
A Novel G Protein-Biased and Subtype-Selective Agonist for a G Protein-Coupled Receptor Discovered from Screening Herbal Extracts.从草药提取物筛选中发现的一种新型G蛋白偶联受体的G蛋白偏向性和亚型选择性激动剂。
ACS Cent Sci. 2020 Feb 26;6(2):213-225. doi: 10.1021/acscentsci.9b01125. Epub 2020 Jan 23.
2
Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT) receptor agonist without 5-HT agonism.设计含氟环丙基取代的 2-苯环丙基甲胺衍生物,鉴定出一种无 5-HT 激动活性的选择性 5-羟色胺 2C(5-HT)受体激动剂。
Eur J Med Chem. 2019 Nov 15;182:111626. doi: 10.1016/j.ejmech.2019.111626. Epub 2019 Aug 14.
3
Pharmabiotics as an Emerging Medication for Metabolic Syndrome and Its Related Diseases.
益生菌作为一种新兴的代谢综合征及其相关疾病治疗药物。
Molecules. 2017 Oct 24;22(10):1795. doi: 10.3390/molecules22101795.
4
Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.发现N-取代的(2-苯基环丙基)甲胺作为功能选择性5-羟色胺2C受体激动剂,有潜力用作抗精神病药物。
J Med Chem. 2017 Jul 27;60(14):6273-6288. doi: 10.1021/acs.jmedchem.7b00584. Epub 2017 Jul 18.
5
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.2-苯环丙基甲胺类化合物作为选择性 5-羟色胺 2C 受体激动剂的优化及其作为潜在抗精神病药物的评估。
J Med Chem. 2015 Feb 26;58(4):1992-2002. doi: 10.1021/jm5019274. Epub 2015 Feb 10.